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Rilpivirine | CAS No: 500287-72-9 | GMP-certified suppliers
A medication that treats HIV-1 infection in antiretroviral-naive and virologically suppressed patients, supporting both oral and long-acting injectable combination regimens.
Therapeutic categories
Primary indications
- Rilpivirine, in combination with other agents, is indicated for the treatment of HIV-1 infections in antiretroviral treatment-naive patients with HIV-1 RNA ≤100,000 copies/mL and CD4+ cell count >200 cells/mm<sup>3</sup>
- The FDA combination therapy approval of rilpivirine and [dolutegravir] is indicated for adults and adolescents 12 years of age and older weighing at least 35 kg with HIV-1 infections whose virus is currently suppressed (< 50 copies/ml) on a stable regimen for at least six months, without a history of treatment failure and no known substitutions associated to resistance to any of the two components of the therapy
- Rilpivirine in combination with [cabotegravir] is indicated as a complete regimen for the treatment of HIV-1 infection in adults and adolescents - ≥12 years old and weighing at least 35kg - to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine
Product Snapshot
- Rilpivirine is available as an oral tablet and intramuscular extended-release suspension formulation
- It is primarily indicated for the treatment of HIV-1 infection in antiretroviral treatment-naive and virologically suppressed patients as part of combination regimens
- Rilpivirine is approved for use in key regulatory markets including the US, Canada, and the EU
Clinical Overview
Pharmacologically, rilpivirine binds non-competitively to the HIV-1 reverse transcriptase enzyme, inhibiting its RNA- and DNA-dependent DNA polymerase activities, thereby blocking viral replication. Unlike nucleoside analogues, rilpivirine does not inhibit human DNA polymerases α, β, or γ. Its molecular structure, characterized by diarylpyrimidine moieties with significant conformational flexibility, permits adaptation to mutations in the reverse transcriptase binding pocket, contributing to sustained antiviral potency and a reduced likelihood of resistance development compared to other NNRTIs.
Rilpivirine demonstrates a favorable pharmacokinetic profile permitting once-daily oral dosing. Additionally, it is available in long-acting intramuscular formulations combined with cabotegravir, enabling dosing intervals of one to two months. Metabolism occurs primarily via cytochrome P450 CYP3A4, and rilpivirine exhibits inhibitory effects on multiple cytochrome P450 enzymes such as CYP2B6, CYP2C19, CYP2C9, and CYP2D6, necessitating careful consideration of drug-drug interactions. The compound is also a substrate and inhibitor of various drug transporters including P-glycoprotein and organic anion transporting polypeptides.
Safety considerations include potential hypersensitivity reactions, hepatotoxicity, depressive disorders, and alterations in body fat distribution. Clinicians and pharmacists should monitor patients for these adverse events during therapy.
Rilpivirine was first approved by the FDA in 2011 and is commercially available in branded formulations including as a single agent and in combination products such as Juluca (rilpivirine with dolutegravir) and Cabenuva (rilpivirine with cabotegravir). These formulations support both oral and injectable treatment paradigms for HIV-1 infection.
From an API sourcing perspective, quality control must ensure high purity and consistent polymorphic form due to rilpivirine’s structural flexibility impacting bioavailability and stability. Compliance with regulatory standards for antiretroviral APIs, including stringent limits on residual solvents and impurities, is critical for global pharmaceutical supply.
Identification & chemistry
| Generic name | Rilpivirine |
|---|---|
| Molecule type | Small molecule |
| CAS | 500287-72-9 |
| UNII | FI96A8X663 |
| DrugBank ID | DB08864 |
Pharmacology
| Summary | Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that non-competitively binds to HIV-1 reverse transcriptase, inhibiting RNA- and DNA-dependent DNA polymerase activities essential for viral replication. Its flexible molecular structure allows adaptation within the reverse transcriptase binding pocket, mitigating resistance development. The compound selectively targets viral enzymes without affecting human DNA polymerases. |
|---|---|
| Mechanism of action | Rilpivirine is a non-competitive NNRTI that binds to reverse transcriptase. Its binding results in the blockage of RNA and DNA- dependent DNA polymerase activities, like HIV-1 replication. It does not present activity against human DNA polymerases α, β and γ. Rilpivirine's flexible structure around the aromatic rings allows the adaptation to changes in the non-nucleoside RT binding pocket, reducing the likelihood of viral mutations conferring resistance. |
| Pharmacodynamics | Rilpivirine is a non-nucleoside reverse transcriptase inhibitor that inhibits the replication of HIV-1. It has a long duration of action as the oral tablet is given daily and the intramuscular suspension is given monthly. Patients should be counselled regarding the risk of hypersensitivity reactions, hepatotoxicity, depressive disorders, and the redistribution or accumulation of body fat. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | inhibitor |
| Nuclear receptor subfamily 1 group I member 2 | Humans | agonist |
ADME / PK
| Absorption | Rilpivirine has a T<sub>max</sub> of 3-4 hours and has a mean AUC of 2235 ± 851 ng\*h/mL. A 25mg dose reaches a C<sub>max</sub> of 247 ng/mL in healthy subjects and 138.6 ng/mL in patients with HIV-1. |
|---|---|
| Half-life | Rilpivirine has a terminal half-life of 34-55 hours. |
| Protein binding | Rilpivirine is >99% bound to plasma protein, most commonly albumin. |
| Metabolism | Rilpivirine is predominantly metabolized by CYP3A4 and CYP3A5 to the hydroxylated metabolites M1, M2, M3, and M4. UGT1A1 glucuronidates the M2 metabolite to form M6, UGT1A4 glucuronidates rilpivirine to form M5, and an unknown UGT glucuronidates the M4 metabolite to form M7. |
| Route of elimination | Rilpivirine is 85% eliminated in the feces and 6.1% eliminated in the urine. 25% of a dose is recovered in the feces as the unchanged parent drug, while <1% of a dose is recovered in the urine as the unchanged parent drug. |
| Volume of distribution | In HIV-1 patients, the apparent volume of distribution in the central compartment was 152-173 L. |
| Clearance | In HIV-1 patients, the apparent total clearance is estimated to be 6.89-8.66 L/h. |
Formulation & handling
- Formulate Rilpivirine as both oral tablets and intramuscular injectable suspensions for extended-release applications.
- Oral administration requires dosing with food to enhance absorption by approximately 40%.
- Avoid co-administration with St. John's Wort due to its potential to reduce systemic drug levels.
Regulatory status
| Lifecycle | The API's key patents in the United States have expired between 2017 and 2021, reflecting a transition to a mature market phase in the US, Canada, and EU. This allows for generic competition and broader product availability across these regions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Rilpivirine is supplied by multiple originator companies with branded products marketed primarily in the US, Canada, and the EU. The presence of several patents, some expiring between 2017 and 2021 in the United States, indicates that generic competition is likely established or emerging in these markets. This landscape supports diversified manufacturing sources for both branded and generic formulations. |
|---|
Safety
| Toxicity | In the event of an overdose, contact a poison control centre. Patients should be treated with symptomatic and supportive measures, including monitoring of the QT interval. Dialysis is not expected to remove significant amounts of the drug from plasma as it is highly bound to albumin. |
|---|
- Rilpivirine exhibits high plasma protein binding, limiting removal by dialysis in overdose scenarios
- Overdose management requires symptomatic and supportive care, including continuous QT interval monitoring
- Handling protocols should consider potential toxicity
Rilpivirine is a type of Anti-HIV
The Anti-HIV category of pharmaceutical APIs comprises a range of active pharmaceutical ingredients (APIs) specifically designed to combat the human immunodeficiency virus (HIV). These APIs play a critical role in the development and production of antiretroviral drugs, which are used to treat HIV infections and prevent the progression to acquired immunodeficiency syndrome (AIDS).
Anti-HIV APIs work by targeting various stages of the HIV life cycle, inhibiting viral replication and reducing the viral load in the body. Some commonly used APIs in this category include nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), and integrase inhibitors (INIs).
NRTIs, such as tenofovir and emtricitabine, act by blocking the reverse transcriptase enzyme, an essential component in the replication of the virus. NNRTIs, such as efavirenz and nevirapine, bind to the reverse transcriptase enzyme, preventing its proper functioning. PIs, like ritonavir and atazanavir, inhibit the protease enzyme, crucial for viral maturation and assembly. INIs, such as raltegravir and dolutegravir, target the integrase enzyme, impeding viral integration into the host's DNA.
These APIs are carefully synthesized and undergo rigorous quality testing to ensure their safety, efficacy, and compliance with regulatory standards. Pharmaceutical companies utilize these APIs as key building blocks to formulate antiretroviral medications, which are then prescribed to individuals living with HIV/AIDS worldwide.
Overall, the Anti-HIV API category plays a vital role in the ongoing battle against HIV/AIDS, offering effective treatment options and improved quality of life for patients affected by this challenging condition.
Rilpivirine API manufacturers & distributors
Compare qualified Rilpivirine API suppliers worldwide. We currently have 11 companies offering Rilpivirine API, with manufacturing taking place in 4 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Acura Labs | Producer | India | India | CoA, GMP | 18 products |
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, USDMF, WC | 98 products |
| Janssen Pharma | Producer | Belgium | Unknown | CoA, GMP, JDMF, USDMF | 63 products |
| Laurus Labs | Producer | India | India | CoA, USDMF | 50 products |
| Minakem | Producer | France | France | CoA, FDA, GMP | 31 products |
| MSN Pharma | Producer | India | India | CoA, USDMF | 31 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shanghai Acebright | Producer | China | China | CoA | 23 products |
| Shanghai Desano Chem. | Producer | China | China | CoA, USDMF | 22 products |
When sending a request, specify which Rilpivirine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Rilpivirine API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
